Derivatives of Iressa, a Specific Epidermal Growth Factor Receptor Inhibitor, are Powerful Apoptosis Inducers in PC3 Prostatic Cancer Cells

The tyrosine kinase activity of the epidermal growth factor receptor (EGFR) is widely involved in signaling pathways and often deregulated in cancer. Its role in the development of prostate cancer is well established, and therapeutic strategies such as blockade of the intracellular tyrosine kinase domain with small‐molecule tyrosine kinase inhibitors have been proposed. Herein we describe the synthesis and in vitro pharmacological properties of C6‐ and C7‐substituted 4‐anilinoquinazolines, analogues of Iressa and powerful proapoptotic inducers in hormone‐independent prostate cancer PC3 cell lines. Synthesis and analysis of the in vitro properties of 4‐anilinoquinazoline derivatives of Iressa, a specific EGFR inhibitor, were carried out. Different relationships are proposed, and the main data is represented by induction of apoptosis in hormone‐independent PC3 cell line.